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» LymeNet Flash » Questions and Discussion » Medical Questions » Artemisinin

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Author Topic: Artemisinin
joysie
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OK, I'm supposed to start this week, adding to amoxy/biaxin/malarone. I promised I have searched...just looking for people's experiences/feedback, you know...the usual.
Thank you
Kris

[ 19. January 2009, 10:30 PM: Message edited by: joysie ]

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CD57
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Artemesinin kicked my butt. But definitely did something. Severe headache within 1/2 hour of taking it.
Don't take it every day, pulse it, or the body makes an enzyme that breaks it down and renders it useless. This per my LLMD. He had me do 4 days on, 3 days off.

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joysie
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Thanks CD-57. How long did it continue to kick your butt ? [Smile] Is it something you acclimate to or suffer and hope things are dying in it's wake?
Thanks
Kris

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CD57
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Hey Joysie, I took it on and off for 4 months and think it helped a lot. It pretty much kicked my butt the whole time. [Smile] I'll probably take it again but will ramp up slower next time.
I'm still unclear as to whether some of what I experienced with it (racing heart, anxiety, headache) was side effect from the art or art killing bugs. How about you?

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lymednva
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I've been on it for over a year now and I didn't notice any big difference when I started it. I do know that I am still somewhat symptomatic and it seems to bring that out in me, sweats balance, especially when herxing.

I was on Mepron and Biaxin with it for the first year, then on Bactrim, with increased dosage of art. Now I'm on Zith with it. I have Babs Duncani, which is hearer to eliminate.

It's different for everyone, so just go ahead and start and see how you do. If it's a problem, pulse it, but I would check with my LLMD before doing that. Just my two cents.

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Lymednva

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joysie
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Thanks lymednva and CD-57. How much did you take? I'm now on 200 mg/day with biaxin, malarone and amoxycillin. I see my LLD today. the past few days have been not so great..we'll see.
Anyone else?
Thanks
Kris

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pingpong
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Hi All,


FWIW,

Heres some considerations, not inclusive, on the effects of artemisia.

Are currently deployed artemisinins neurotoxic?

Stephen Toovey
Royal Free and University College Medical School, London, UK
Travel Clinic, Cape Town, South Africa

Received 28 April 2006; revised 31 May 2006; accepted 1 June 2006. Available online 7 June 2006.


Abstract

In vitro, animal, and human clinical studies suggest currently deployed artemisinins possess neurotoxic potential. A specific and consistent pattern of brainstem injuries that includes auditory processing centers has been reported from all laboratory animals studied. Hearing loss, ataxia, and tremor are reported from humans. Neurotoxicity appears mediated in part through artemisinin induced oxidative stress in exposed brainstems. In vitro studies suggest that artemisinin neurotoxicity does not manifest immediately upon exposure, but that once commenced it is inevitable and irreversible; extrapolation from in vitro data suggests that 14 days may possibly be required for full development, casting doubt upon some animal safety studies and human necropsy studies. Uncertainty remains over the neurotoxicity of currently deployed artemisinins, and their safety profile should be reviewed, especially in pediatric use. The development of non-neurotoxic artemisinins is possible and should be encouraged.

Keywords: Artemisinin; Artemether
________________________________________
http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?db=pubmed&cmd=Retrieve&dopt=AbstractPlus&list_uids=14757313&query_hl=4&itool=pubmed_docsum

Toxicol Lett. 2004 Mar 1;147(2):99-107. Links
Comment in:
Toxicol Lett. 2004 Aug 1;151(3):489-90, author reply 491-2.
Artemisinin derivatives: toxic for laboratory animals, safe for humans?Gordi T, Lepist EI.
Department of Pharmaceutics, School of Pharmacy, State University of New York at Buffalo, Buffalo, NY 14260, USA. [email protected]

A discrepancy seems to prevail with regard to the toxicity and safety of the artemisinin family of antimalarials. While these compounds have been found to be virtually void of any serious side effects in humans, their neurotoxicity in animal models has raised concerns about their use. In this paper, we present selected examples of both pre-clinical and clinical studies dealing with adverse effects of artemisinin drugs. We suggest that the prolonged presence of artemisinins upon slow release from oil-based intramuscular formulations is the main cause of the observed toxicity in laboratory animals. In contrast, oral intake of these compounds, which is by far the most common formulation used for treatment of malaria patients, results in rapid clearance of these drugs and is thus unlikely to cause any toxicity in human subjects. Another plausible factor may be the relatively high doses of artemisinin compounds used in animal studies. In conclusion, the observation of the toxicity of artemisinin compounds in animals, but not in humans, is most likely due to different pharmacokinetic profiles after different routes of administrations.

PMID: 14757313

Med Trop (Mars). 1998;58(3 Suppl):32-7. Links
Neurotoxicity and artemisinin compounds do the observations in animals justify limitation of clinical use?Dayan AD.
Department of Toxicology, Saint Bartholomew's School of Medicine, London, United Kingdom. [email protected]

High parenteral doses of certain artemisinin derivatives can produce a limited and unique, ******selective brain stem neuronopathy in laboratory animals.**** There is necrosis of a small number of nerve cells in certain brain stem nuclei and more extensive chromatolysis of neurons in the same nuclei a few days after *****intramuscular or intravenous injection of dihydroqinghaosu, artemether and arteether in doses exceeding about 6mg/kg/d intramuscular or intravenous for about 3-5 days (in an oily solvent) in the dog, or after a single parenteral dose exceeding about 100 mg/kg. The limited information available about the monkey suggests that it is only affected after doses several times higher. The probable order of sensitivity of species is dog > rat > monkey, but this is based on only few results. No lesions have been reported after various intramuscular and oral dosages of artesunate and artelinate. The limited reports of clinical observations have not suggested any specific pattern of abnormalities. The lesion is unique in its distribution, in the small number of neurons that become necrotic and the occurrence in nearby cells of chromatolysis. The latter is almost certainly reversible because more prolonged or higher dose studies have not shown more extensive neuronal damage. As the pathogenesis of this toxic response is not known, evaluation of the risk to man must be based on conventional assessment of active doses in animals versus those employed in the treatment of cerebral malaria. It is argued that there is no reason to anticipate a particular risk of conventional regimes employing up to artemether 3-6mg/kg/d intramuscular or other regimes involving artesunate per rectum for a few days.

PMID: 10212895

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pingpong

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